Our Science – Ambudkar Website

Suresh V. Ambudkar, Ph.D.

Selected Publications

1) Gardner ER, Ahlers CM, Shukla S, Sissung TM, Ockers SB, Price DK, Hamada A, Robey RW, Steinberg SM, Ambudkar SV, Dahut WL, Figg WD.
Association of the ABCG2 C421A polymorphism with prostate cancer risk and survival.
BJU Int. 2008. [Journal]

2) Wu C, Calcagno AM, Ambudkar S.
Reversal of ABC drug transporter-mediated multidrug resistance in cancer cells: Evaluation of current strategies.
Current Molecular Pharmacology. 1: 93-105, 2008. [Journal]

3) Tsai CJ, Sauna ZE, Kimchi-Sarfaty C, Ambudkar SV, Gottesman MM, Nussinov R.
Synonymous Mutations and Ribosome Stalling Can Lead to Altered Folding Pathways and Distinct Minima.
J. Mol. Biol. 2008. [Journal]

4) Henrich C, Bokesch H, Bates S, Robey R, Shukla S, Ambudkar S, Dean M, McMahon J, inventor; DHHS, assignee.
Method of inhibiting ABCG2 and related treatments methods.
Patent Pending, Filed in 2008. Application No. 61/018,758. Pending [Patent]

5) Henrich C, Bokesch H, Bates S, Robey R, Shukla S, Ambudkar S, Dean M, McMahon J, inventor; DHHS, assignee.
Method of inhibiting ABCG2 and related treatments.
Patent Pending, Filed in 2007. Application No. 60/986,155. Pending [Patent]

6) Wright MH, Calcagno AM, Salcido CD, Carlson MD, Ambudkar SV, Varticovski L.
Brca1 breast tumors contain distinct CD44+/CD24- and CD133+ cells with cancer stem cell characteristics.
Breast Cancer Res. 10: R10, 2008. [Journal]

7) Shukla S, Wu CP, Ambudkar SV.
Development of inhibitors of ATP-binding cassette drug transporters: present status and challenges.
Expert opinion on drug metabolism & toxicology. 4: 205-23, 2008. [Journal]

8) Shukla S, Sauna ZE, Ambudkar SV.
Evidence for the interaction of imatinib at the transport-substrate site(s) of the multidrug-resistance-linked ABC drug transporters ABCB1 (P-glycoprotein) and ABCG2.
Leukemia. 22: 445-447, 2008. [Journal]

9) Robey RW, Shukla S, Finley EM, Oldham RK, Barnett D, Ambudkar SV, Fojo T, Bates SE.
Inhibition of P-glycoprotein (ABCB1)- and multidrug resistance-associated protein 1 (ABCC1)-mediated transport by the orally administered inhibitor, CBT-1((R)).
Biochem. Pharmacol. 75: 1302-1312, 2008. [Journal]

10) Kim IW, Booth-Genthe C, Ambudkar SV.
Relationship Between Drugs and Functional Activity of Various Mammalian P-Glycoproteins (ABCB1).
Mini reviews in medicinal chemistry. 8: 193-200, 2008. [Journal]

11) Calcagno AM, Fostel JM, To KK, Salcido CD, Martin SE, Chewning KJ, Wu CP, Varticovski L, Bates SE, Caplen NJ, Ambudkar SV.
Single-step doxorubicin-selected cancer cells overexpress the ABCG2 drug transporter through epigenetic changes.
Br. J. Cancer. 98: 1515-24, 2008. [Journal]

12) Chen SY, Pan CJ, Nandigama K, Mansfield BC, Ambudkar SV, Chou JY.
The glucose-6-phosphate transporter is a phosphate-linked antiporter deficient in glycogen storage disease type Ib and Ic.
FASEB J. 2008. [Journal]

13) Kimchi-Sarfaty C, Oh JM, Kim IW, Sauna ZE, Calcagno AM, Ambudkar SV, Gottesman MM.
A.
Science. 315: 525-8, 2007. [Journal]

14) Calcagno AM, Kim IW, Wu CP, Shukla S, Ambudkar SV.
ABC drug transporters as molecular targets for the prevention of multidrug resistance and drug-drug interactions.
Current drug delivery. 4: 324-33, 2007. [Journal]

15) Sauna ZE, Ambudkar SV.
About a switch: how P-glycoprotein (ABCB1) harnesses the energy of ATP binding and hydrolysis to do mechanical work.
Mol. Cancer Ther. 6: 13-23, 2007. [Journal]

16) Sauna ZE, Kim IW, Nandigama K, Kopp S, Chiba P, Ambudkar SV.
Catalytic Cycle of ATP Hydrolysis by P-Glycoprotein: Evidence for Formation of the E.S Reaction Intermediate with ATP-gamma-S, a Nonhydrolyzable Analogue of ATP.
Biochemistry. 46: 13787-13799, 2007. [Journal]

17) Golin J, Kon ZN, Wu CP, Martello J, Hanson L, Supernavage S, Ambudkar SV, Sauna ZE.
Complete inhibition of the Pdr5p multidrug efflux pump ATPase activity by its transport substrate clotrimazole suggests that GTP as Well as ATP may be used as an energy source.
Biochemistry. 46: 13109-19, 2007. [Journal]

18) Shi Z, Peng XX, Kim IW, Shukla S, Si QS, Robey RW, Bates SE, Shen T, Ashby CR, Fu LW, Ambudkar SV, Chen ZS.
Erlotinib (Tarceva, OSI-774) antagonizes ATP-binding cassette subfamily B member 1 and ATP-binding cassette subfamily G member 2-mediated drug resistance.
Cancer Res. 67: 11012-20, 2007. [Journal]

19) Wu CP, Shukla S, Calcagno AM, Hall MD, Gottesman MM, Ambudkar SV.
Evidence for dual mode of action of a thiosemicarbazone, NSC73306: a potent substrate of the multidrug resistance linked ABCG2 transporter.
Mol. Cancer Ther. 6: 3287-96, 2007. [Journal]

20) Sauna ZE, Kim IW, Ambudkar SV.
Genomics and the mechanism of P-glycoprotein (ABCB1).
J Bioenerg Biomembr. 2007. [Journal]

21) Paterson JK, Shukla S, Black CM, Tachiwada T, Garfield S, Wincovitch S, Ernst DN, Agadir A, Li X, Ambudkar SV, Szakacs G, Akiyama SI, Gottesman MM.
Human ABCB6 Localizes to Both the Outer Mitochondrial Membrane and the Plasma Membrane.
Biochemistry. 2007. [Journal]

22) Brendel C, Scharenberg C, Dohse M, Robey RW, Bates SE, Shukla S, Ambudkar SV, Wang Y, Wennemuth G, Burchert A, Boudriot U, Neubauer A.
Imatinib mesylate and nilotinib (AMN107) exhibit high-affinity interaction with ABCG2 on primitive hematopoietic stem cells.
Leukemia. 21: 1267-75, 2007. [Journal]

23) Robey RW, Shukla S, Steadman K, Obrzut T, Finley EM, Ambudkar SV, Bates SE.
Inhibition of ABCG2-mediated transport by protein kinase inhibitors with a bisindolylmaleimide or indolocarbazole structure.
Mol. Cancer Ther. 6: 1877-85, 2007. [Journal]

24) Henrich CJ, Robey RW, Bokesch HR, Bates SE, Shukla S, Ambudkar SV, Dean M, McMahon JB.
New inhibitors of ABCG2 identified by high-throughput screening.
Mol. Cancer Ther. 6: 3271-8, 2007. [Journal]

25) Sauna ZE, Kimchi-Sarfaty C, Ambudkar SV, Gottesman MM.
Silent polymorphisms speak: how they affect pharmacogenomics and the treatment of cancer.
Cancer Res. 67: 9609-12, 2007. [Journal]

26) Shi Z, Jain S, Kim IW, Peng XX, Abraham I, Youssef DT, Fu LW, El Sayed K, Ambudkar SV, Chen ZS.
Sipholenol A, a marine-derived sipholane triterpene, potently reverses P-glycoprotein (ABCB1)-mediated multidrug resistance in cancer cells.
Cancer Sci. 98: 1373-80, 2007. [Journal]

27) Shukla S, Wu CP, Nandigama K, Ambudkar SV.
The naphthoquinones, vitamin K3 and its structural analogue plumbagin, are substrates of the multidrug resistance linked ATP binding cassette drug transporter ABCG2.
Mol. Cancer Ther. 6: 3279-86, 2007. [Journal]

28) Sauna ZE, Kimchi-Sarfaty C, Ambudkar SV, Gottesman MM.
The sounds of silence: synonymous mutations affect function.
Pharmacogenomics. 8: 527-532, 2007. [Journal]

29) Golin J, Ambudkar SV, May L.
The yeast Pdr5p multidrug transporter: how does it recognize so many substrates?.
Biochem. Biophys. Res. Commun. 356: 1-5, 2007. [Journal]

30) Calcagno AM, Ludwig JA, Fostel JM, Gottesman MM, Ambudkar SV.
Comparison of drug transporter levels in normal colon, colon cancer, and Caco-2 cells: impact on drug disposition and discovery.
Mol. Pharm. 3: 87-93, 2006. [Journal]

31) Rai V, Gaur M, Shukla S, Shukla S, Ambudkar SV, Komath SS, Prasad R.
Conserved Asp327 of walker B motif in the N-terminal nucleotide binding domain (NBD-1) of Cdr1p of Candida albicans has acquired a new role in ATP hydrolysis.
Biochemistry. 45: 14726-39, 2006. [Journal]

32) Pawarode A, Shukla S, Minderman H, Fricke SM, Pinder EM, O'loughlin KL, Ambudkar SV, Baer MR.
Differential effects of the immunosuppressive agents cyclosporin A, tacrolimus and sirolimus on drug transport by multidrug resistance proteins.
Cancer Chemother Pharmacol. 2006. [Journal]

33) Sauna ZE, Nandigama K, Ambudkar SV.
Exploiting reaction intermediates of the ATPase reaction to elucidate the mechanism of transport by P-glycoprotein (ABCB1).
J. Biol. Chem. 281: 26501-11, 2006. [Journal]

34) Limtrakul P, Chearwae W, Shukla S, Phisalphong C, Ambudkar SV.
Modulation of function of three ABC drug transporters, P-glycoprotein (ABCB1), mitoxantrone resistance protein (ABCG2) and multidrug resistance protein 1 (ABCC1) by tetrahydrocurcumin, a major metabolite of curcumin.
Mol Cell Biochem. 2006. [Journal]

35) Chearwae W, Shukla S, Limtrakul P, Ambudkar SV.
Modulation of the function of the multidrug resistance-linked ATP-binding cassette transporter ABCG2 by the cancer chemopreventive agent curcumin.
Mol. Cancer Ther. 5: 1995-2006, 2006. [Journal]

36) Calcagno AM, Chewning KJ, Wu CP, Ambudkar SV.
Plasma membrane calcium ATPase (PMCA4): A housekeeper for RT-PCR relative quantification of polytopic membrane proteins.
BMC Mol Biol. 7: 29, 2006. [Journal]

37) Seamon JA, Rugg CA, Emanuel S, Calcagno AM, Ambudkar SV, Middleton SA, Butler J, Borowski V, Greenberger LM.
Role of the ABCG2 drug transporter in the resistance and oral bioavailability of a potent cyclin-dependent kinase/Aurora kinase inhibitor.
Mol. Cancer Ther. 5: 2459-67, 2006. [Journal]

38) Ludwig JA, Szakács G, Martin SE, Chu BF, Cardarelli C, Sauna ZE, Caplen NJ, Fales HM, Ambudkar SV, Weinstein JN, Gottesman MM.
Selective toxicity of NSC73306 in MDR1-positive cells as a new strategy to circumvent multidrug resistance in cancer.
Cancer Res. 66: 4808-15, 2006. [Journal]

39) Ambudkar SV, Kim IW, Xia D, Sauna ZE.
The A-loop, a novel conserved aromatic acid subdomain upstream of the Walker A motif in ABC transporters, is critical for ATP binding.
FEBS Lett. 580: 1049-55, 2006. [Journal]

40) Shukla S, Robey RW, Bates SE, Ambudkar SV.
The calcium channel blockers, 1,4-dihydropyridines, are substrates of the multidrug resistance-linked ABC drug transporter, ABCG2.
Biochemistry. 45: 8940-51, 2006. [Journal]

41) Kim IW, Peng XH, Sauna ZE, Fitzgerald PC, Xia D, Müller M, Nandigama K, Ambudkar SV.
The Conserved Tyrosine Residues 401 and 1044 in ATP Sites of Human P-Glycoprotein Are Critical for ATP Binding and Hydrolysis: Evidence for a Conserved Subdomain, the A-Loop in the ATP-Binding Cassette.
Biochemistry. 45: 7605-16, 2006. [Journal]

42) Ambudkar SV, Kim IW, Sauna ZE.
The power of the pump: mechanisms of action of P-glycoprotein (ABCB1).
European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences. 27: 392-400, 2006. [Journal]

43) Ambudkar SV, Sauna ZE, Gottesman MM, Szakacs G.
A novel way to spread drug resistance in tumor cells: functional intercellular transfer of P-glycoprotein (ABCB1).
Trends Pharmacol Sci. 2005. [Journal]

44) Chearwae W, Wu CP, Chu HY, Lee TR, Ambudkar SV, Limtrakul P.
Curcuminoids purified from turmeric powder modulate the function of human multidrug resistance protein 1 (ABCC1).
Cancer Chemother Pharmacol. 1-13, 2005. [Journal]

45) Wu CP, Klokouzas A, Hladky SB, Ambudkar SV, Barrand MA.
Interactions of mefloquine with ABC proteins, MRP1 (ABCC1) and MRP4 (ABCC4) that are present in human red cell membranes.
Biochem Pharmacol. 70: 500-10, 2005. [Journal]

46) Wu CP, Calcagno AM, Hladky SB, Ambudkar SV, Barrand MA.
Modulatory effects of plant phenols on human multidrug-resistance proteins 1, 4 and 5 (ABCC1, 4 and 5).
FEBS J. 272: 4725-40, 2005. [Journal]

47) Jiang Y, Bhattacharjee H, Zhou T, Rosen BP, Ambudkar SV, Sauna ZE.
Nonequivalence of the nucleotide binding domains of the ArsA ATPase.
J Biol Chem. 280: 9921-6, 2005. [Journal]

48) Hanson L, May L, Tuma P, Keeven J, Mehl P, Ferenz M, Ambudkar SV, Golin J.
The role of hydrogen bond acceptor groups in the interaction of substrates with Pdr5p, a major yeast drug transporter.
Biochemistry. 44: 9703-13, 2005. [Journal]

49) Sauna ZE, Andrus MB, Turner TM, Ambudkar SV.
Biochemical basis of polyvalency as a strategy for enhancing the efficacy of P-glycoprotein (ABCB1) modulators: stipiamide homodimers separated with defined-length spacers reverse drug efflux with greater efficacy.
Biochemistry. 43: 2262-71, 2004. [Journal]

50) Chearwae W, Anuchapreeda S, Nandigama K, Ambudkar SV, Limtrakul P.
Biochemical mechanism of modulation of human P-glycoprotein (ABCB1) by curcumin I, II, and III purified from Turmeric powder.
Biochem Pharmacol. 68: 2043-52, 2004. [Journal]

51) Shukla S, Sauna ZE, Prasad R, Ambudkar SV.
Disulfiram is a potent modulator of multidrug transporter Cdr1p of Candida albicans.
Biochem Biophys Res Commun. 322: 520-5, 2004. [Journal]

52) Sauna ZE, Nandigama K, Ambudkar SV.
Multidrug resistance protein 4 (MRP4/ABCC4)-mediated ATP hydrolysis: Effect of transport substrates and characterization of the post-hydrolysis transition state.
J Biol Chem. 2004. [Journal]

53) Polgar O, Robey RW, Morisaki K, Dean M, Michejda C, Sauna ZE, Ambudkar SV, Tarasova N, Bates SE.
Mutational analysis of ABCG2: role of the GXXXG motif.
Biochemistry. 43: 9448-56, 2004. [Journal]

54) Shukla S, Ambudkar SV, Prasad R.
Substitution of threonine-1351 in the multidrug transporter Cdr1p of Candida albicans results in hypersusceptibility to antifungal agents and threonine-1351 is essential for synergic effects of calcineurin inhibitor FK520.
J Antimicrob Chemother. 54: 38-45, 2004. [Journal]

55) Sauna ZE, Peng XH, Nandigama K, Tekle S, Ambudkar SV.
The molecular basis of the action of disulfiram as a modulator of the multidrug resistance-linked ATP binding cassette transporters MDR1 (ABCB1) and MRP1 (ABCC1).
Mol Pharmacol. 65: 675-84, 2004. [Journal]

56) Singh BB, Lockwich TP, Bandyopadhyay BC, Liu X, Bollimuntha S, Brazer SC, Combs C, Das S, Leenders AG, Sheng ZH, Knepper MA, Ambudkar SV, Ambudkar IS.
VAMP2-dependent exocytosis regulates plasma membrane insertion of TRPC3 channels and contributes to agonist-stimulated Ca2+ influx.
Mol Cell. 15: 635-46, 2004. [Journal]

57) Shukla S, Saini P, Smriti , Jha S, Ambudkar SV, Prasad R.
Functional characterization of Candida albicans ABC transporter Cdr1p.
Eukaryot Cell. 2: 1361-75, 2003. [Journal]

58) Ambudkar SV, Kimchi-Sarfaty C, Sauna ZE, Gottesman MM.
P-glycoprotein: from genomics to mechanism.
Oncogene. 22: 7468-85, 2003. [Journal]

59) Golin J, Ambudkar SV, Gottesman MM, Habib AD, Sczepanski J, Ziccardi W, May L.
Studies with novel Pdr5p substrates demonstrate a strong size dependence for xenobiotic efflux.
J Biol Chem. 278: 5963-9, 2003. [Journal]

60) Kozak L, Gopal G, Yoon JH, Sauna ZE, Ambudkar SV, Thakurta AG, Dhar R.
Elf1p, a member of the ABC class of ATPases, functions as a mRNA export factor in Schizosacchromyces pombe.
J Biol Chem. 277: 33580-9, 2002. [Journal]

61) Müller M, Yong M, Peng XH, Petre B, Arora S, Ambudkar SV.
Evidence for the role of glycosylation in accessibility of the extracellular domains of human MRP1 (ABCC1).
Biochemistry. 41: 10123-32, 2002. [Journal]

62) Sauna ZE, Müller M, Peng XH, Ambudkar SV.
Importance of the conserved Walker B glutamate residues, 556 and 1201, for the completion of the catalytic cycle of ATP hydrolysis by human P-glycoprotein (ABCB1).
Biochemistry. 41: 13989-4000, 2002. [Journal]

63) Anuchapreeda S, Leechanachai P, Smith MM, Ambudkar SV, Limtrakul PN.
Modulation of P-glycoprotein expression and function by curcumin in multidrug-resistant human KB cells.
Biochem Pharmacol. 64: 573-82, 2002. [Journal]

64) Kimchi-Sarfaty C, Kasir J, Ambudkar SV, Rahamimoff H.
Transport activity and surface expression of the Na+-Ca2+ exchanger NCX1 are inhibited by the immunosuppressive agent cyclosporin A and by the nonimmunosuppressive agent PSC833.
J Biol Chem. 277: 2505-10, 2002. [Journal]

65) Sauna ZE, Ambudkar SV.
Characterization of the catalytic cycle of ATP hydrolysis by human P-glycoprotein. The two ATP hydrolysis events in a single catalytic cycle are kinetically similar but affect different functional outcomes.
J Biol Chem. 276: 11653-61, 2001. [Journal]

66) Kerr KM, Sauna ZE, Ambudkar SV.
Correlation between steady-state ATP hydrolysis and vanadate-induced ADP trapping in Human P-glycoprotein. Evidence for ADP release as the rate-limiting step in the catalytic cycle and its modulation by substrates.
J Biol Chem. 276: 8657-64, 2001. [Journal]

67) Sauna ZE, Smith MM, Müller M, Kerr KM, Ambudkar SV.
The mechanism of action of multidrug-resistance-linked P-glycoprotein.
J Bioenerg Biomembr. 33: 481-91, 2001. [Journal]

68) Sauna ZE, Ambudkar SV.
Evidence for a requirement for ATP hydrolysis at two distinct steps during a single turnover of the catalytic cycle of human P-glycoprotein.
Proc Natl Acad Sci U S A. 97: 2515-20, 2000. [Journal]

69) Andrus MB, Turner TM, Sauna ZE, Ambudkar SV.
The synthesis and evaluation of a solution phase indexed combinatorial library of non-natural polyenes for reversal of P-glycoprotein mediated multidrug resistance.
J Org Chem. 65: 4973-83, 2000. [Journal]

This page was last updated on 9/18/2008.